Design and synthesis of novel small molecule N/OFQ receptor antagonists

Zhengming Chen; R Richard Goehring; Kenneth J Valenzano; Donald J Kyle

doi:10.1016/j.bmcl.2003.11.083

Design and synthesis of novel small molecule N/OFQ receptor antagonists

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1347-51. doi: 10.1016/j.bmcl.2003.11.083.

Authors

Zhengming Chen¹, R Richard Goehring, Kenneth J Valenzano, Donald J Kyle

Affiliation

¹ Drug Discovery, Purdue Pharma L.P., 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. zhengming.chen@pharma.com

PMID: 14980696
DOI: 10.1016/j.bmcl.2003.11.083

Abstract

Small molecule N/OFQ receptor antagonists were designed and synthesized to further investigate the therapeutic potential of N/OFQ receptor modulators. The resulting octahydrobenzimidazol-2-ones 14 and 23 show excellent antagonistic activity towards both N/OFQ and mu receptors with high affinity to the human N/OFQ receptor.

MeSH terms

Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology*
Drug Design*
Humans
Narcotic Antagonists*
Nociceptin Receptor
Piperidines / chemical synthesis*
Piperidines / pharmacology*
Protein Binding
Receptors, Opioid

Substances

Benzimidazoles
J 113397
Narcotic Antagonists
Piperidines
Receptors, Opioid
Nociceptin Receptor
OPRL1 protein, human